Page last updated: 2024-11-04

loxoprofen

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is used to relieve pain and inflammation. It is a derivative of propionic acid, and it is available as both a racemate and as the S-enantiomer. Loxoprofen is thought to work by inhibiting the production of prostaglandins, which are chemicals that cause pain and inflammation. Loxoprofen is used to treat a variety of conditions, including rheumatoid arthritis, osteoarthritis, and pain associated with menstrual cramps. It is also used to reduce fever. Loxoprofen is available in both oral and topical forms. It is generally well-tolerated, but it can cause side effects such as gastrointestinal upset, headache, and dizziness. Loxoprofen is not recommended for use in people who are allergic to aspirin or other NSAIDs. Loxoprofen is an important drug for treating pain and inflammation, and it is widely used around the world. It is studied to understand its mechanisms of action, to improve its effectiveness, and to develop new drugs that are more effective and have fewer side effects.'

loxoprofen: RN given refers to parent cpd without isomeric designation; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

loxoprofen : A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID3965
CHEMBL ID19299
CHEBI ID76172
SCHEMBL ID24423
MeSH IDM0120978

Synonyms (78)

Synonym
AC-15776
EU-0100677
loxoprofen, solid
loxoprofeno [spanish]
loxoprofen
loxoprofenum [latin]
(+-)-p-((2-oxocyclopentyl)methyl)hydratropic acid
loxoprofene [french]
loxoprofen [inn]
LOPAC0_000677
NCGC00094037-01
NCGC00094037-02
NCGC00015594-02
koloxo
L 0664
NCGC00015594-04
2-[4-(2-oxo-cyclopentylmethyl)-phenyl]-propionic acid
bdbm50140320
CHEMBL19299 ,
loxoprofen acid
chebi:76172 ,
loxoprofen (inn)
D08149
68767-14-6
2-[4-[(2-oxocyclopentyl)methyl]phenyl]propanoic acid
A836244
HMS3262G15
loxoprofeno
loxoprofenum
unii-3583h0gzap
3583h0gzap ,
loxoprofene
cas-68767-14-6
tox21_110178
dtxcid9025164
dtxsid1045164 ,
CCG-204763
S4682
NCGC00015594-03
FT-0641207
LP00677
AKOS015906359
2-(4-((2-oxocyclopentan-1-yl)methyl)phenyl)propionic acid
loxoprofen [who-dd]
loxoprofen [mi]
(+/-)-p-((2-oxocyclopentyl)methyl)hydratropic acid
HY-B0578
2-(4-((2-oxocyclopentyl)methyl)phenyl)propanoic acid
SCHEMBL24423
NCGC00263577-01
2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid
(+-)-((2-oxocyclopentyl)methyl)hydratropic acid
tox21_110178_1
2-[4-(2-oxocyclopentan-1-ylmethyl)phenyl]-propionic acid
2-[4-(2-oxocyclopentan-1-ylmethyl)phenyl]propionic acid
tox21_500677
NCGC00261362-01
Q-300011
Q-201324
benzeneacetic acid, .alpha.-methyl-4-[(2-oxocyclopentyl)methyl]-
alpha-methyl-4-[(2-oxocyclopentyl)methyl]benzeneacetic acid
mfcd00864331
DB09212
GS-3193
AC-8108
sr-01000075955
SR-01000075955-1
Q2759348
SY113439
2-[4-[(2-oxocyclopentyl)methyl]phenyl]propionic acid
L0244
BCP10971
cs-600; cs600; cs 600
SDCCGSBI-0050656.P002
HMS3885N16
NCGC00015594-08
2-(4-((2-oxocyclopentyl)methyl)-phenyl)propanoic acid
EN300-249698

Research Excerpts

Overview

Loxoprofen is a non-steroidal anti-inflammatory drug of the 2-arylpropionic acid type. It has been used to treat musculoskeletal disorders in the horse racing industry. The active trans-alcohol metabolite is produced in the liver by carbonyl reductase.

ExcerptReferenceRelevance
"Loxoprofen tromethamine is a novel structural compound related to loxoprofen. "( Embryo-fetal developmental toxicity and toxicokinetics of loxoprofen tromethamine intravenously administered to pregnant rats.
Gao, Q; Liu, J; Lu, F; Qiao, H; Yue, P; Zhao, X, 2023
)
2.6
"Loxoprofen is a non-steroidal anti-inflammatory drug of the 2-arylpropionic acid type, which has used to treat musculoskeletal disorders in the horse racing industry. "( Analysis of loxoprofen in tablets, patches, and equine urine as tert-butyldimethylsilyl derivative by gas chromatography-mass spectrometry.
Ji, M; Jung, S; Kim, H; Kim, M; Kim, Y; Kwak, J; Lee, G; Lee, HS; Lee, W; Oh, S; Paik, MJ; Park, HJ; Seo, C; Sin, E; Yu, J, 2018
)
2.3
"Loxoprofen is an anti-inflammatory drug that requires bioactivation into the trans-OH metabolite to exert pharmacological activity. "( CBR1 rs9024 genotype status impacts the bioactivation of loxoprofen in human liver.
Atilla-Gokcumen, GE; Blanco, JG; Del Solar, V; Li, N; Quiñones-Lombraña, A, 2018
)
2.17
"Loxoprofen (LOX) is a nonsteroidal anti-inflammatory drug (NSAID). "( Efficacy and Safety of Loxoprofen Hydrogel Transdermal Patch Versus Loxoprofen Tablet in Chinese Patients with Myalgia: A Double-Blind, Double-Dummy, Parallel-Group, Randomized, Controlled, Non-Inferiority Trial.
Chen, Z; Hu, S; Li, Z; Lin, J; Shao, Z; Shi, Y; Wang, G; Xiao, W; Zhang, Z; Zhao, D; Zheng, Y, 2019
)
2.27
"Loxoprofen is a prodrug that exerts strong analgesic and anti-inflammatory effects through its active trans-alcohol metabolite, which is produced in the liver by carbonyl reductase. "( Identification of sulfonyl-loxoprofen as novel phase 2 conjugate in rat.
Cho, P; Jeong, TC; Lee, ES; Lee, S; Lee, T; Paudel, S; Shrestha, A; Shrestha, R, 2019
)
2.25
"1. Loxoprofen (LX), is a prodrug of the pharmacologically active form, trans-alcohol metabolite (trans-OH form), which shows very potent analgesic effect. "( Absorption, distribution, metabolism and excretion of loxoprofen after dermal application of loxoprofen gel to rats.
Izumi, T; Kazui, M; Kurihara, A; Sawamura, R, 2014
)
1.27
"Loxoprofen (LOXO) is a non-steroidal anti-inflammatory drug. "( The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen.
Fang, L; Hui, M; Quan, P; Yang, Y, 2016
)
2.1
"Loxoprofen is a prodrug nonselective NSAID developed to protect upper gastrointestinal tract."( Celecoxib Monotherapy Maintained Small Intestinal Mucosa Better Compared With Loxoprofen Plus Lansoprazole Treatment: A Double-blind, Randomized, Controlled Trial.
Fujimori, S; Hanada, R; Hayashida, M; Ikushima, I; Sakamoto, C; Sakurai, T, 2016
)
1.38
"Loxoprofen is a nonsteroidal anti-inflammatory drug used in the treatment of many diseases. "( Loxoprofen-induced interstitial pneumonia: a case report.
Arano, N; Jo, H; Kato, M; Kuriyama, S; Muraki, K; Nagashima, O; Sasaki, S; Sekimoto, Y; Suina, K; Takahashi, K; Tominaga, S; Yoshioka, Y, 2016
)
3.32
"Loxoprofen sodium (LOX) is a recently developed novel propionic acid derivative. "( Identification and Structure Elucidation of Forced Degradation Products of the Novel Propionic acid Derivative Loxoprofen: Development of Stability-Indicating Chromatographic Methods Validated as per ICH Guidelines.
Abd El-Sattar, OI; Eissa, MS, 2017
)
2.11
"Loxoprofen sodium is an effective treatment for some patients with refractory nocturia."( Loxoprofen sodium treatment for elderly men with refractory nocturia: effect on night-time urine production.
Kohri, K; Kojima, Y; Okada, S; Sasaki, S; Watanabe, H; Yanai, Y, 2008
)
2.51

Toxicity

ExcerptReferenceRelevance
") occurring after the start of rabeprazole treatment were handled as adverse events."( Efficacy and safety of rabeprazole in non-steroidal anti-inflammatory drug-induced ulcer in Japan.
Mizokami, Y, 2009
)
0.35
"Non-steroidal anti-inflammatory drugs (NSAIDs) are an effective and common treatment for chronic pain disorders, but long-term use is associated with risk of potentially life-threatening gastrointestinal adverse events (AEs)."( Safety and efficacy of long-term esomeprazole 20 mg in Japanese patients with a history of peptic ulcer receiving daily non-steroidal anti-inflammatory drugs.
Kinoshita, Y; Miwa, H; Sugano, K; Takeuchi, T, 2013
)
0.39
"Because oral nonsteroidal anti-inflammatory drugs (NSAIDs) have adverse effects on kidney function, patients with kidney diseases are administered these drugs as transdermal patches."( Safety and efficacy of skin patches containing loxoprofen sodium in diabetic patients with overt nephropathy.
Araki, H; Araki, S; Isshiki, K; Kashiwagi, A; Kume, S; Kuwagata, S; Maegawa, H; Morita, Y; Soumura, M; Uzu, T; Yamahara, K, 2014
)
0.66
" A lower incidence of adverse events was observed in LX-P group; however, the difference was not statistically significant."( Efficacy and safety of loxoprofen hydrogel patch versus loxoprofen tablet in patients with knee osteoarthritis: a randomized controlled non-inferiority trial.
Bao, CD; Chen, ZW; Hu, SX; Li, YJ; Li, ZG; Mu, R; Shao, ZW; Wang, GC; Xiao, WG; Zhang, W; Zhang, ZY; Zhao, DB; Zheng, Y, 2016
)
0.74
" No serious adverse events occurred in either group."( Efficacy and Safety of Loxoprofen Hydrogel Transdermal Patch Versus Loxoprofen Tablet in Chinese Patients with Myalgia: A Double-Blind, Double-Dummy, Parallel-Group, Randomized, Controlled, Non-Inferiority Trial.
Chen, Z; Hu, S; Li, Z; Lin, J; Shao, Z; Shi, Y; Wang, G; Xiao, W; Zhang, Z; Zhao, D; Zheng, Y, 2019
)
0.82
" However, oral nonsteroidal anti-inflammatory drugs cause several adverse events, with topical formulations arising as an important alternative."( Efficacy and safety of loxoprofen sodium topical patch for the treatment of pain in patients with minor acute traumatic limb injuries in Brazil: a randomized, double-blind, noninferiority trial.
Daher, MT; Fujiki, EN; Kraychete, DC; Lopes, DG; Nakamoto, A; Netto, NA; Tardini, R, 2019
)
0.82
" There were four secondary outcomes, including the extent of pain relief, the change trends of VAS scores, joint function scores measured by the Western Ontario and McMaster University Osteoarthritis Index (WOMAC), and adverse events."( Efficacy and safety of flurbiprofen cataplasms versus loxoprofen sodium cataplasms in knee osteoarthritis: a randomized controlled trial.
Cheng, Y; Guan, Z; Jia, J; Kan, J; Li, D; Liu, J; Wang, Z; Wu, Z; Xue, T; Yuan, P; Zhai, S; Zhang, G; Zhang, H; Zhang, K, 2023
)
1.16
" In addition, the FPC group experienced a significantly lower incidence of adverse events (5."( Efficacy and safety of flurbiprofen cataplasms versus loxoprofen sodium cataplasms in knee osteoarthritis: a randomized controlled trial.
Cheng, Y; Guan, Z; Jia, J; Kan, J; Li, D; Liu, J; Wang, Z; Wu, Z; Xue, T; Yuan, P; Zhai, S; Zhang, G; Zhang, H; Zhang, K, 2023
)
1.16

Pharmacokinetics

ExcerptReferenceRelevance
" This method was successfully applied to the pharmacokinetic study of loxoprofen in human volunteers following a single oral administration of loxoprofen sodium (60 mg, anhydrate) tablet."( Direct and simultaneous analysis of loxoprofen and its diastereometric alcohol metabolites in human serum by on-line column switching liquid chromatography and its application to a pharmacokinetic study.
Cho, HY; Lee, YB; Park, CH, 2006
)
0.84
" The several pharmacokinetic parameters were evaluated after an oral administration after an overnight fast according to a single dose, two-sequence, and cross-over randomized design with a 1-week washout interval."( Pharmacokinetics and bioequivalence study of two brands of loxoprofen tablets in healthy volunteers.
Jhee, OH; Kang, JS; Lee, MH; Lee, SE; Park, JH; Shaw, LM, 2007
)
0.58
" Overall, the pharmacokinetic characteristics of F-LOX, including the formation of metabolites in vivo and in vitro, were comparable to those of LOX."( Comparison of pharmacokinetics between loxoprofen and its derivative with lower ulcerogenic activity, fluoro-loxoprofen.
Maruyama, T; Mizushima, T; Ohtsuka, M; Okamoto, Y; Suemasu, S; Tahara, K; Tanaka, K; Watanabe, H; Yamakawa, N, 2013
)
0.66
" The objective of the present study was to develop an IVIVC approach based on population pharmacokinetic (POP-PK) modeling that incorporated physiologically relevant absorption kinetics."( Development of a Physiologically Relevant Population Pharmacokinetic in Vitro-in Vivo Correlation Approach for Designing Extended-Release Oral Dosage Formulation.
Bulitta, JB; Kim, TH; Shin, BS; Shin, S; Yoo, SD; Youn, YS, 2017
)
0.46

Compound-Compound Interactions

Silver needle heat conduction therapy combined with loxoprofen sodium can effectively treat KOA. Its mechanism may be related to alleviating inflammation and improving bone metabolism.

ExcerptReferenceRelevance
"Little is known about the effects of drug-drug interactions between valacyclovir and non-steroidal anti-inflammatory drugs (NSAIDs)."( Acute kidney injury during concomitant use of valacyclovir and loxoprofen: detecting drug-drug interactions in a spontaneous reporting system.
Jiang, P; Shi, J; Sun, H; Yue, Z, 2014
)
0.64
" Combined with penetration enhancers, the cumulative amounts were further increased in presence of 5% IPM, which exhibited a flux of 840."( The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen.
Fang, L; Hui, M; Quan, P; Yang, Y, 2016
)
0.65
"To observe the clinical efficacy of silver needle heat conduction therapy combined with loxoprofen sodium patch in the treatment of knee osteoarthritis (KOA)."( [Therapeutic effect and mechanism of silver needle heat conduction therapy combined with loxoprofen sodium patch in patients with knee osteoarthritis].
Han, J; Ling, DY; Wang, ZY; Wu, CX; Zhang, ZW, 2021
)
1.07
" Patients of the combination group were treated with silver needle heat conduction therapy combined with loxoprofen sodium patch, while those of the loxoprofen sodium group were treated with loxoprofen sodium patch."( [Therapeutic effect and mechanism of silver needle heat conduction therapy combined with loxoprofen sodium patch in patients with knee osteoarthritis].
Han, J; Ling, DY; Wang, ZY; Wu, CX; Zhang, ZW, 2021
)
1.06
"Silver needle heat conduction therapy combined with loxoprofen sodium can effectively treat KOA, its mechanism may be related to alleviating inflammation and improving bone metabolism."( [Therapeutic effect and mechanism of silver needle heat conduction therapy combined with loxoprofen sodium patch in patients with knee osteoarthritis].
Han, J; Ling, DY; Wang, ZY; Wu, CX; Zhang, ZW, 2021
)
1.09
"To explore the efficacy of glucosamine sulfate (GS) combined with loxoprofen sodium (LS) in rats with knee osteoarthritis (KOA) and its effect on chondrocytes."( The inhibiting effect of glucosamine sulfate combined with loxoprofen sodium on chondrocyte apoptosis in rats with knee osteoarthritis.
Luo, M; Luo, W; Wang, Q; Xu, F, 2021
)
1.1
"GS combined with LS showed good efficacy in rats with knee osteoarthritis, which may be achieved by inhibiting the expression of inflammatory factors and knee chondrocyte apoptosis via the TLR4-NF-kB pathway."( The inhibiting effect of glucosamine sulfate combined with loxoprofen sodium on chondrocyte apoptosis in rats with knee osteoarthritis.
Luo, M; Luo, W; Wang, Q; Xu, F, 2021
)
0.86

Bioavailability

ExcerptReferenceRelevance
" These results indicate that the present method is very simple and readily applicable to routine bioavailability studies of these compounds with an acceptable sensitivity."( Simultaneous determination of loxoprofen and its diastereomeric alcohol metabolites in human plasma and urine by a simple HPLC-UV detection method.
Choo, KS; Chung, SJ; Jung, JK; Kim, IW; Lee, MH; Shim, CK; Suh, YG, 2001
)
0.6
" In addition, in vivo oral bioavailability was found to decrease with prolonged drug dissolution, indicating site-specific absorption."( Development of a Physiologically Relevant Population Pharmacokinetic in Vitro-in Vivo Correlation Approach for Designing Extended-Release Oral Dosage Formulation.
Bulitta, JB; Kim, TH; Shin, BS; Shin, S; Yoo, SD; Youn, YS, 2017
)
0.46
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Nanoemulsions (NEs) are one type of delivery system that helps to improve the solubility and dissolution of drugs, attempting to enhance their bioavailability and onset of action."( Development of omega-3 loxoprofen-loaded nanoemulsion to limit the side effect associated with NSAIDs in treatment of tooth pain.
Abualsunun, WA; Alhakamy, NA; Alkhalidi, HM; Almehmady, AM; Alruwaili, NK; Bakhaidar, RB; Hassan, AH; Hosny, KM; Khallaf, RA; Khames, A; Kurakula, M; Rizg, WY; Sindi, AM, 2021
)
0.93

Dosage Studied

ExcerptRelevanceReference
" Furthermore, to assess time profiles of KP concentration in the skin and plasma, guinea pigs received a repeated topical application of R-KP and S-KP at a dosage of 40 mg/kg over a period of 3 days."( Study on the mechanism of photosensitive dermatitis caused by ketoprofen in the guinea pig.
Chikamatsu, N; Igarashi, T; Nagata, O; Nakazawa, T; Shimo, T; Yamamoto, M, 2006
)
0.33
"579), the rescue dosage rate (p=0."( A Comparison of Analgesic Effect between Loxoprofen and Celecoxib and the Frequency of the Hemorrhage Following Tonsillectomy.
Ariki, M; Fukushima, N; Hirai, T; Miyahara, N; Yoshiga, A, 2016
)
0.7
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitorA compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
monocarboxylic acidAn oxoacid containing a single carboxy group.
cyclopentanonesAny alicyclic ketone that consists of a cyclopentane skeleton substituted by at least one oxo group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
endonuclease IVEscherichia coliPotency17.78280.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.00640.100020.879379.4328AID488772; AID588453; AID588456
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.36490.01237.983543.2770AID1645841
estrogen nuclear receptor alphaHomo sapiens (human)Potency15.08900.000229.305416,493.5996AID743075
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.00080.001628.015177.1139AID1259385
chromobox protein homolog 1Homo sapiens (human)Potency39.81070.006026.168889.1251AID488953
heat shock protein beta-1Homo sapiens (human)Potency1.49590.042027.378961.6448AID743210
huntingtin isoform 2Homo sapiens (human)Potency15.84890.000618.41981,122.0200AID2673
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency79.43280.010323.856763.0957AID2662
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)100.00000.00021.557410.0000AID161659
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)100.00000.00010.995010.0000AID162650
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (60)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (85)

Assay IDTitleYearJournalArticle
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID162663Inhibitory potency against cyclooxygenase-2 in human whole blood assay2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
AID676449Inhibition of LPS-stimulated human whole blood COX-2 assessed as inhibition of PGE2 production at 10 uM by EIA2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID676456Toxicity in rat assessed as gastric ulcerogenic activity at 0.37 to 7.45 mM/kg, po measured after 8 hrs2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID161659Inhibitory activity against recombinant human prostaglandin G/H synthase 12004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID179451Analgesic activity on peroral administration against Scald induced pain in rat paw1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID676453Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX22012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID161672Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID676454Antiinflammatory activity against Wistar rat assessed as inhibition of carrageenan induced edema volume at 37.3 uM/kg, po administered 1 hr prior carrageenan-challenge measured after 3 hrs post challenge2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID162650Inhibitory activity against recombinant human Prostaglandin G/H synthase 22004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID676238Inhibition of human whole blood COX-1 assessed as inhibition of TXB2 production at 10 uM by EIA2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID676455Antiinflammatory activity against Wistar rat assessed as inhibition of carrageenan induced edema volume at 37.3 uM/kg, po administered 1 hr prior carrageenan-challenge measured after 6 hrs post challenge2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID676239Inhibition of human whole blood COX-1 assessed as inhibition of TXB2 production at 100 uM by EIA2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID676450Inhibition of LPS-stimulated human whole blood COX-2 assessed as inhibition of PGE2 production at 100 uM by EIA2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID182609Antiinflammatory activity on peroral administration against carrageenan paw edema1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (235)

TimeframeStudies, This Drug (%)All Drugs %
pre-199010 (4.26)18.7374
1990's16 (6.81)18.2507
2000's59 (25.11)29.6817
2010's114 (48.51)24.3611
2020's36 (15.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 69.23

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index69.23 (24.57)
Research Supply Index5.66 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index118.42 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (69.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials41 (16.80%)5.53%
Reviews7 (2.87%)6.00%
Case Studies54 (22.13%)4.05%
Observational2 (0.82%)0.25%
Other140 (57.38%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (16)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Autologous Platelet Rich Plasma in Ultrasound Guided Intervertebral Disk Injection Therapy for Chronic Low Back Pain [NCT02983747]112 participants (Anticipated)Interventional2019-11-01Recruiting
A Phase 2, Randomized, Double-Blind, Parallel-Group and Placebo-Controlled Pilot Study to Assess the Safety and Efficacy of a New Pain Patch Versus Placebo and No Treatment for the Treatment of Delayed Onset Muscle Soreness (DOMS) [NCT02602353]Phase 242 participants (Actual)Interventional2015-10-31Completed
A Phase III, Randomized, Double Blind, Non-inferiority, Comparative Study of the New Transdermal Patch Dosage Form Containing Loxoprofen Sodium (100 mg) and Loxonin® (60 mg Tablet) for the Treatment of Acute Traumatic Injuries [NCT02616068]Phase 3242 participants (Actual)Interventional2015-10-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Phase 4 Study To Compare The Effect Of Celecoxib 100 Mg BID, Loxoprofen 60 Mg TID And Placebo On The Gastroduodenal Mucosa In Healthy Subjects [NCT00994461]Phase 4190 participants (Actual)Interventional2009-11-30Completed
A Single-Centre, Open, Randomised, Three-Way Cross-Over Drug-Drug Interaction Study of Esomeprazole (D961H) Capsule and Loxoprofen Tablet After Repeated Oral Administration in Japanese Healthy Male Subjects [NCT00676117]Phase 130 participants (Anticipated)Interventional2008-04-30Completed
Non-Steroidal Anti-inflammatory Drugs (NSAIDS) vs. Tramadol in Pain Management After Transnasal Transsphenoidal Surgery Among Patients With Pituitary Adenomas: A Prospective Randomized Controlled Trial [NCT04611685]202 participants (Anticipated)Interventional2020-10-31Recruiting
A Multicenter, Randomized, Single Blind, Positive Drug and Placebo Parallel Controlled Phase II Clinical Trial to Evaluate the Efficacy and Safety of HRF2105patch in Relieving Pain of Osteoarthritis [NCT06047483]Phase 290 participants (Anticipated)Interventional2023-10-31Not yet recruiting
Clinical Trial to Evaluate the Efficacy of Bee Venom Acupuncture on Chronic Low Back Pain [NCT01491321]Phase 254 participants (Anticipated)Interventional2011-04-30Recruiting
A Randomized, Multicenter, Active And Placebo Controlled Parallel Group Study To Evaluate The Efficacy And Safety Of Celecoxib (Ym177) 200 Bid Compared To Loxoprofen 60 Mg Tid In Patients With Low Back Pain [NCT00141154]Phase 31,234 participants (Actual)Interventional2004-10-31Completed
Clinical Research on the Efficacy and Safety of East-West Collaborative Treatment Using NSAIDs and BV on Chronic Cervical Pain; A Randomized, Controlled, Parallel, Pilot Study [NCT01922466]Phase 260 participants (Anticipated)Interventional2013-07-31Completed
Efficacy and Safety of Loxoprofen Hydrogel Patch Versus Loxoprofen Tablet in Patients With Ankylosing Spondylitis: a 4-week Randomized, Open-label Study [NCT03800797]Phase 470 participants (Actual)Interventional2015-05-25Completed
[NCT01779271]Phase 3183 participants (Actual)Interventional2013-01-31Completed
A Randomized, Double Blind, Placebo-controlled Pilot-study to Evaluate Efficacy and Safety of Low-dose hrIL-2 in the Treatment of Methotrexate (MTX)-Naive Patients With Rheumatoid Arthritis [NCT02467504]Phase 247 participants (Actual)Interventional2015-07-01Completed
Open-label, Single-group, Multicentre, Phase III Study to Confirm the Efficacy and Safety of IP-TN When Administered for 2 Weeks to Patients With Low Back Pain, Scapulohumeral Periarthritis, or Cervico-omo-brachial Syndrome Associated With Muscle Strain [NCT02831569]Phase 380 participants (Actual)Interventional2016-07-27Completed
An in Vivo Bioequivalence Study of FABALOFEN 60 (Loxoprofen Sodium 60mg/Tablet) of Pharbaco Central Pharmaceutical J.S.C No.I With JAPROLOX® TABLETS (Loxoprofen Sodium 60mg/Tablet) of Daiichi Sankyo Propharma Co., Ltd [NCT04386122]Phase 124 participants (Actual)Interventional2020-05-07Completed
Clinical Research on the Efficacy and Safety of Bosinji on LBP and Radiculopathy by HIVD of L-spine; A Multicenter, Randomized, Controlled, Clinical Trial [NCT03386149]Phase 374 participants (Actual)Interventional2017-12-28Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00994461 (7) [back to overview]Incidence of Gastroduodenal Ulcers
NCT00994461 (7) [back to overview]Incidence of Treatment-emergent, All-causality GI Body System Adverse Events
NCT00994461 (7) [back to overview]Incidence of Any Gastric, and Duodenal Ulcers
NCT00994461 (7) [back to overview]Incidence of Any Gastroduodenal, Gastric, and Duodenal Ulcers and/or Erosions
NCT00994461 (7) [back to overview]Number of Gastroduodenal Erosions in Each Subject
NCT00994461 (7) [back to overview]Number of Gastroduodenal Ulcers in Each Subject
NCT00994461 (7) [back to overview]Post-treatment Gastroduodenal Endoscopic Scores (According to Mucosal Grading Scale)
NCT02467504 (20) [back to overview]Number of Participants With Adverse Events
NCT02467504 (20) [back to overview]Percentage of Participants Achieving DAS28 Remission.
NCT02467504 (20) [back to overview]C Reactive Protein (CRP)
NCT02467504 (20) [back to overview]Erythrocyte Sedimentation Rate (ESR)
NCT02467504 (20) [back to overview]Percentage of CD4+ Treg Cells
NCT02467504 (20) [back to overview]Percentage of Participants Achieving a Good or Moderate European League Against Rheumatism (EULAR) Response
NCT02467504 (20) [back to overview]Percentage of Participants Achieving DAS28 Low Disease Activity.
NCT02467504 (20) [back to overview]Percentage of Participants Meeting the 2011 American College of Rheumatology/ European League Against Rheumatism (ACR/EULAR) Remission Criteria Simplified for Clinical Practice
NCT02467504 (20) [back to overview]Percentage of Participants Meeting the American College of Rheumatology 20% Response Criteria
NCT02467504 (20) [back to overview]Percentage of Participants Meeting the American College of Rheumatology 50% Response Criteria
NCT02467504 (20) [back to overview]Percentage of Participants Meeting the American College of Rheumatology 70% Response Criteria
NCT02467504 (20) [back to overview]The Change From Baseline of a Health Assessment Questionnaire- Disability Index (HAQ-DI)
NCT02467504 (20) [back to overview]The Change From Baseline of Clinical Disease Activity Index (CDAI)
NCT02467504 (20) [back to overview]The Change From Baseline of Patient's Assessment of Arthritis Pain (PtAAP)
NCT02467504 (20) [back to overview]The Change From Baseline of Patient's Global Assessment of Disease Activity (PtGADA)
NCT02467504 (20) [back to overview]The Change From Baseline of Physician's Global Assessment of Disease Activity (PhGADA)
NCT02467504 (20) [back to overview]The Change From Baseline of Simplified Disease Activity Index (SDAI)
NCT02467504 (20) [back to overview]The Scores of SF-36 Quetionnaire
NCT02467504 (20) [back to overview]Work Productivity Survey - Rheumatoid Arthritis [WPS-RA]
NCT02467504 (20) [back to overview]Work Productivity Survey - Rheumatoid Arthritis [WPS-RA]-2
NCT02831569 (2) [back to overview]Assessment of Pain Due to Low Back Pain, Scapulohumeral Periarthritis or Cervico-omo-brachial Syndrome After 2 Weeks of Treatment
NCT02831569 (2) [back to overview]Percentage of Patients With Drug-related Adverse Events [AEs]

Incidence of Gastroduodenal Ulcers

The percentage of subjects who had gastroduodenal endoscopic ulcers after 2 weeks treatment (The number of subjects who had gastroduodenal endoscopic ulcers after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. (NCT00994461)
Timeframe: 2 weeks

InterventionPercent (Number)
Celecoxib1.4
Loxoprofen27.6
Placebo2.7

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Incidence of Treatment-emergent, All-causality GI Body System Adverse Events

The percentage of subjects who had treatment-emergent, all-causality gastrointestinal body system adverse events after 2 weeks treatment (The number of subjects who had treatment-emergent, all-causality gastrointestinal body system adverse events after 2 weeks treatment divided by participants multiplied by 100.) (NCT00994461)
Timeframe: 2 weeks

InterventionPercent (Number)
Celecoxib24.3
Loxoprofen47.4
Placebo16.2

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Incidence of Any Gastric, and Duodenal Ulcers

The percentage of subjects who had gastric and duodenal endoscopic ulcers after 2 weeks treatment (The number of subjects who had gastric and duodenal endoscopic ulcers after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. (NCT00994461)
Timeframe: 2 weeks

,,
InterventionPercent (Number)
Gastric ulcersDuodenal ulcers
Celecoxib01.4
Loxoprofen25.05.3
Placebo2.70

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Incidence of Any Gastroduodenal, Gastric, and Duodenal Ulcers and/or Erosions

The percentage of subjects who had gastroduodenal, gastric, and duodenal endoscopic ulcers and/or erosions after 2 weeks treatment (The number of subjects who had gastroduodenal, gastric, and duodenal endoscopic ulcers and/or erosions after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. An erosion is defined as a lesion producing a definite break in the mucosa with equivocal depth. (NCT00994461)
Timeframe: 2 weeks

,,
InterventionPercent (Number)
Gastroduodenal ulcers and/or erosionsGastric ulcers and/or erosionsDuodenal ulcers and/or erosions
Celecoxib36.535.14.1
Loxoprofen53.953.95.3
Placebo24.324.30

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Number of Gastroduodenal Erosions in Each Subject

Number of subjects for each number of gastroduodenal endoscopic erosions after 2 weeks treatment (An erosion is defined as a lesion producing a definite break in the mucosa with equivocal depth.) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
0 erosion1 erosion2 erosions3 erosions4 erosions5 erosions6 erosions7 erosions8 erosions9 erosions10 or more erosions
Celecoxib4714450021001
Loxoprofen4113394311100
Placebo295120000000

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Number of Gastroduodenal Ulcers in Each Subject

Number of subjects for each number of gastroduodenal endoscopic ulcers after 2 weeks treatment (An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth.) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
0 ulcer1 ulcer2 ulcers3 ulcers4 ulcers5 ulcers6 ulcers7 ulcers8 ulcers9 ulcers10 or more ulcers
Celecoxib731000000000
Loxoprofen5510520012100
Placebo361000000000

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Post-treatment Gastroduodenal Endoscopic Scores (According to Mucosal Grading Scale)

Number of subjects for each gastroduodenal endoscopic score (according to Mucosal Grading Scale) after 2 weeks treatment (Score 0 = normal mucosa (no visible lesions); Score 1 = 1 to 10 petechiae; Score 2 = more than 10 petechiae; Score 3 = 1 to 5 erosions; Score 4 = 6 to 10 erosions; Score 5 = 11 to 25 erosions; Score 6 = more than 25 erosions; Score 7 = ulcer) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
Score 0Score 1Score 2Score 3Score 4Score 5Score 6Score 7
Celecoxib3881224001
Loxoprofen33201910021
Placebo226080001

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Number of Participants With Adverse Events

adverse events includes injection site reactions, influenza-like symptoms, infection, fever, tumor, cardiovascular event, drug-induced liver and kidney damage. (NCT02467504)
Timeframe: Up to week 24

InterventionParticipants (Count of Participants)
Experimental11
Placebo Comparator9

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Percentage of Participants Achieving DAS28 Remission.

DAS 28 remission is defined by a disease activity score (28 joint) calculated using the erythrocyte sedimentation rate (DAS28-ESR) of less than 2.6 (NCT02467504)
Timeframe: week 24

InterventionParticipants (Count of Participants)
Experimental6
Placebo Comparator6

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C Reactive Protein (CRP)

(NCT02467504)
Timeframe: week 12, week 24

,
Interventionmg/L (Mean)
week 24week 12
Experimental21.69.5
Placebo Comparator15.327.8

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Erythrocyte Sedimentation Rate (ESR)

(NCT02467504)
Timeframe: week 12, week 24

,
Interventionmillimeter/hour (Mean)
Week 24Week 12
Experimental43.329.6
Placebo Comparator36.828.3

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Percentage of CD4+ Treg Cells

analysis regulatory CD4+ T(Treg) cells before and during IL-2 treatment. P values<0.05 are considered statistically significant. (NCT02467504)
Timeframe: week 12, week 24

,
Interventionpercentage of CD4+ T cells (Mean)
Week 24Week 12
Experimental6.946.84
Placebo Comparator6.465.37

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Percentage of Participants Achieving a Good or Moderate European League Against Rheumatism (EULAR) Response

"Good response is defined as: DAS28-ESR ≤ 3.2 and decrease from Baseline by > 1.2.~moderate response is defined as achievement of one of the following: DAS28-ESR ≤ 3.2 and decrease from Baseline > 0.6 and ≤ 1.2 DAS28-ESR > 3.2 and ≤ 5.1 and decrease from Baseline > 0.6 DAS28-ESR > 5.1 and decrease from Baseline >1.2." (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24week 12
Experimental1715
Placebo Comparator2014

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Percentage of Participants Achieving DAS28 Low Disease Activity.

Low disease activity is defined by a disease activity score (28 joint) calculated using the erythrocyte sedimentation rate (DAS28-ESR) of less than 3.2 (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24week 12
Experimental87
Placebo Comparator97

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Percentage of Participants Meeting the 2011 American College of Rheumatology/ European League Against Rheumatism (ACR/EULAR) Remission Criteria Simplified for Clinical Practice

The 2011 ACR/EULAR remission criteria simplified for clinical practice is defined as:Tender Joint Count (TJC) ≤ 1, Swollen Joint Count (SJC) ≤ 1 and Patient's Global Assessment of Disease Activity (PtGADA) ≤ 1. (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24week 12
Experimental20
Placebo Comparator10

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Percentage of Participants Meeting the American College of Rheumatology 20% Response Criteria

The assessments are based on a 20% or greater improvement from Baseline in the number of tender joints, a 20%, or more improvement in the number of swollen joints, and a 20% or greater improvement in 3 of the 5 remaining core set measures: Patient's Global Assessment of Disease Activity (PtGADA), Physician's Global Assessment of Disease Activity (PhGADA), Patient's Assessment of Arthritis Pain (PtAAP), physical function as assessed by the Health Assessment Questionnaire - Disability Index (HAQ-DI) and C-Reactive Protein (CRP). (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24week 12
Experimental1312
Placebo Comparator1310

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Percentage of Participants Meeting the American College of Rheumatology 50% Response Criteria

The assessments are based on a 50% or greater improvement from Baseline in the number of tender joints, a 50%, or more improvement in the number of swollen joints, and a 50% or greater improvement in 3 of the 5 remaining core set measures: Patient's Global Assessment of Disease Activity (PtGADA), Physician's Global Assessment of Disease Activity (PhGADA), Patient's Assessment of Arthritis Pain (PtAAP), physical function as assessed by the Health Assessment Questionnaire - Disability Index (HAQ-DI) and C-Reactive Protein (CRP). (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24weed 12
Experimental106
Placebo Comparator83

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Percentage of Participants Meeting the American College of Rheumatology 70% Response Criteria

The assessments are based on a 70% or greater improvement from Baseline in the number of tender joints, a 70%, or more improvement in the number of swollen joints, and a 70% or greater improvement in 3 of the 5 remaining core set measures: Patient's Global Assessment of Disease Activity (PtGADA), Physician's Global Assessment of Disease Activity (PhGADA), Patient's Assessment of Arthritis Pain (PtAAP), physical function as assessed by the Health Assessment Questionnaire - Disability Index (HAQ-DI) and C-Reactive Protein (CRP). (NCT02467504)
Timeframe: week 12, week 24

,
InterventionParticipants (Count of Participants)
week 24week 12
Experimental42
Placebo Comparator20

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The Change From Baseline of a Health Assessment Questionnaire- Disability Index (HAQ-DI)

"The domains of the HAQ-DI are dressing and grooming, arising, eating, walking, hygiene, reach, grip and common daily activities. The total score ranges from 0 to 3 with lower scores meaning lower disability.~The change from baseline of HAQ-DI, minimum is -3, the maximum is 3. higher scores mean a worse outcome." (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-0.63-0.50
Placebo Comparator-0.38-0.25

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The Change From Baseline of Clinical Disease Activity Index (CDAI)

"Clinical Disease Activity Index(CDAI), the minimum is 0, the maximum is 76. higher scores mean a worse outcome.~The change of from baseline of CDAI, the minimum is -76, the maximum is 76. higher scores mean a worse outcome." (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-17.5-15.0
Placebo Comparator-11-8.0

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The Change From Baseline of Patient's Assessment of Arthritis Pain (PtAAP)

VAS score from 0 to 100 for Patient's Assessment of Arthritis Pain higher scores mean a worse outcome. The change from baseline of PtAAP, the minimum is -100, the maximum is 100. (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-57.5-57.1
Placebo Comparator-33.3-27.3

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The Change From Baseline of Patient's Global Assessment of Disease Activity (PtGADA)

VAS score from 0 to 100 for Patient's Global Assessment of Disease Activity Higher scores mean a worse outcome. The change from baseline of PtGADA, the minimum is -100, the maximum is 100. Higher scores mean a worse outcome. (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-57.5-57.1
Placebo Comparator-33.3-33.3

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The Change From Baseline of Physician's Global Assessment of Disease Activity (PhGADA)

VAS score from 0 to 100 for Physician's Global Assessment of Disease Activity higher scores mean a worse outcome. The change from baseline, the minimum is -100, the maximum is 100. (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-58.3-57.1
Placebo Comparator-44.4-25.0

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The Change From Baseline of Simplified Disease Activity Index (SDAI)

"Simplified Disease Activity Index(SDAI). the minimum is 0, the maximum is 96. higher scores mean worse outcome.~The change from baseline of SDAI. the minimum is -96, the maximum is 96. higher scores mean worse outcome." (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental-19.0-16.9
Placebo Comparator-12.1-9.2

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The Scores of SF-36 Quetionnaire

Score ranging from 0 to 100 with higher scores a better outcome. (NCT02467504)
Timeframe: week 12, week 24

,
Interventionscore on a scale (Median)
week 24week 12
Experimental15.2924.32
Placebo Comparator6.9027.25

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Work Productivity Survey - Rheumatoid Arthritis [WPS-RA]

The Arthritis interference in the last month with work productivity is measured on a scale that ranges from 0 (no interference) to 10 (complete interference). The Arthritis interference in the last month with household work productivity is measured on a scale that ranges from 0 (no interference) to 10 (complete interference).higher scores mean a worse outcome. (NCT02467504)
Timeframe: week 24

,
Interventionunits on a scale (Median)
rate of Arthritis interferenceRate of arthritis interference with household work
Experimental35
Placebo Comparator25

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Work Productivity Survey - Rheumatoid Arthritis [WPS-RA]-2

In the last month, number of work days missed, number of work days with reduced productivity. In the last month, number of days with no household work, number of days with reduced household work productivity, number of days with hired outside help, number of days missed of family/social/leisure activities in the last month.higher scores mean a worse outcome. (NCT02467504)
Timeframe: week 24

,
Interventiondays (Median)
number of work days with reduced productivitynumber of work days missedHousehold work days missed due to arthritisDays with household work productivity reducedDays with activities missed due to arthritisDays with outside help hired due to arthritis
Experimental3.5001550
Placebo Comparator0001200

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Assessment of Pain Due to Low Back Pain, Scapulohumeral Periarthritis or Cervico-omo-brachial Syndrome After 2 Weeks of Treatment

"The outcome measure presents percentage of patients who showed marked improvement or moderate improvement in low back pain and/or scapulohumeral periarthritis and/or cervico-omo-brachial syndrome after 2 weeks of treatment." (NCT02831569)
Timeframe: Post 2 weeks.

InterventionPercentage of participants (Number)
Loxoprofen Sodium/Methocarbamol [FDC]37.5

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